ML375，5MG，SML2728-5MG，Sigma

Biochem/physiol Actions

ML375 is an orally active, brain-penetrant, potent and M5 subtype-selective muscarinic acetylcholine receptor (mAChR) negative allosteric modulator (NAM) (IC₅₀ = 300/790 nM against 10 μM NMS-induced Ca²⁺ mobilization in h/r M5-transfected CHO cells; h/r M1-M4 IC₅₀ >30 μM) that reduces N-methylscopolamine (NMS) ML5 dissociation rate without competing against NMS for receptor binding. M375 shows in vivo efficacy in rat models of substances addiction (cocaine, ethanol, oxycodone) with excellent multispecies pharmacokinetic properties.
Orally active, brain-penetrant, potent & M5-selective muscarinic acetylcholine receptor (mAChR) NAM with in vivo efficacy in rat models of substances addiction.